(S)-H-1152 (hydrochloride)

Rho-associated kinase (ROCK), activated by GTP-linked Rho, phosphorylates targets that are involved in cytoskeletal remodeling, smooth muscle contraction, and neuronal development. H-1152 is a potent, specific, ATP-competitive, and cell permeable inhibitor of ROCK (Ki = 1.6 nM).{17660}{17661} It is a more potent inhibitor of ROCK than either Y-27632 (Ki = 140 nM) or HA-1077 (Ki = 330 nM).{17661} H-1152 poorly inhibits PKA, PKC, and myosin light chain kinase (Ki = 0.63, 9.27, and 10.1 ?M, respectively).{17661} It has been used to examine the role of ROCK in such diverse processes as stress fiber assembly,{17662} vasoconstriction,{17663} as well as spontaneously tonic smooth muscle{17664} and neurite extension.{17665}